Sustained release of lidocaine from Poloxamer 407 gels
Sustained release of lidocaine from Poloxamer 407 gels
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DOI：
10.1016/j.ijpharm.2004.09.028
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发表时间：
2005-01-20
影响因子：
5.8
通讯作者：
Marchetti, JM
中科院分区：
文献类型：
--
作者：
Ricci, EJ;Lunardi, LO;Marchetti, JM
在这项工作中，我们表明，改变P407凝胶含量可以影响药物释放速率。P407凝胶制剂中通常包含的无机盐和PEG 400也可以改变药物释放的速率。选择利多卡因作为模型药物是因为，尽管利多卡因广泛用于治疗疼痛，但其使用受到其作用持续时间短的限制。P407的使用缩短了利多卡因在注射部位的停留时间，维持药物释放并增加治疗效果。在扩散系统中进行释放研究。在释放过程中，数据遵循Higuchi平方根定律时间动力学（r>0.98）。凝胶中聚合物浓度的增加会增加粘度，并通过延长凝胶溶解时间和延长药物通过凝胶基质的扩散来降低利多卡因释放速率和扩散系数。在NaCl或PEG 400水溶液组成的凝胶中，利多卡因的释放速率和扩散系数增加。由于这些添加剂是亲水性的，它们减少了凝胶溶解时间，从而加速了药物扩散。泊洛沙姆具有生物相容性，结果支持使用泊洛沙姆凝胶作为缓释注射制剂的可能性。(C)2004 Elsevier B.V.保留所有权利。
In this work, we show that alteration of P407 gel content can affect drug release rates. The inorganic salts and PEG 400 commonly included in the formulation of P407 gels can also change the rate at which a drug is released. Lidocaine was selected as a model drug because, although widely used in the treatment of pain, its use is limited by short duration of its effects. The use of P407 gets prolongs the residence time of the lidocaine at the injection site, sustains drug release and increases therapeutic efficacy. Release studies were performed in a diffusion system. During release, data followed the Higuchi square root law time kinetic (r>0.98). Increased polymer concentration in the gel increases viscosity and reduces lidocaine release rates and diffusion coefficients via extended gel dissolution time and prolonged drug diffusion through the gel matrix. Lidocaine release rates and diffusion coefficients increased in gels composed of NaCl or PEG 400 aqueous solution. Because these additives are hydrophilic, they reduce gel dissolution time, thereby accelerating drug diffusion. Poloxamer is biocompatible and the results support the possibility of using Poloxamer gel as a sustained release injectable formulation. (C) 2004 Elsevier B.V. All rights reserved.